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Amido-Isothiazole Compounds and Their Use as Inhibitors of 11Beta-HSD1 for the Treatment of Metabolic Syndrome and Related Disorders

a technology of amidoisothiazole and compounds, which is applied in the field of therapeutic compounds, can solve the problems of a substantial risk of cardiovascular diseas

Inactive Publication Date: 2012-04-19
THE UNIV COURT OF THE UNIV OF EDINBURGH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

These abnormalities confer a substantial risk of cardiovascular disease.

Method used

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  • Amido-Isothiazole Compounds and Their Use as Inhibitors of 11Beta-HSD1 for the Treatment of Metabolic Syndrome and Related Disorders
  • Amido-Isothiazole Compounds and Their Use as Inhibitors of 11Beta-HSD1 for the Treatment of Metabolic Syndrome and Related Disorders
  • Amido-Isothiazole Compounds and Their Use as Inhibitors of 11Beta-HSD1 for the Treatment of Metabolic Syndrome and Related Disorders

Examples

Experimental program
Comparison scheme
Effect test

examples of specific embodiments

[0621]In one embodiment, the compounds are selected from compounds of the following formulae and pharmaceutically acceptable salts, hydrates, and solvates thereof:

Code No.SynthesisStructureAA-0123AA-0224

[0622]In one embodiment, the compounds are selected from compounds of the following formulae and pharmaceutically acceptable salts, hydrates, and solvates thereof:

Code No.SynthesisStructureBB-017BB-0213BB-034

[0623]In one embodiment, the compounds are selected from compounds of the following formulae and pharmaceutically acceptable salts, hydrates, and solvates thereof:

CodeNo.SynthesisStructureCC-0116CC-0212

Substantially Purified Forms

[0624]One aspect of the present invention pertains to AITZ compounds, as described herein, in substantially purified form and / or in a form substantially free from contaminants.

[0625]In one embodiment, the compound is in substantially purified form and / or in a form substantially free from contaminants.

[0626]In one embodiment, the compound is in a substant...

examples

[0728]The following examples are provided solely to illustrate the present invention and are not intended to limit the scope of the invention, as described herein.

Analytical Method 1:

[0729]The system consisted of a Hewlett Packard HP1100 LC system and a Higgins Clipeus 5 μm C18 100×3.0 mm column. Detection was achieved using a Micromass ZQ quadrupole electrospray (positive and negative ion), a UV detector at 254 nm and a Sedex ELS 85 evaporative light scattering detector. Mobile Phase A: 0.1% aqueous formic acid, Mobile Phase B: 0.1% formic acid in MeCN. Flow rate 1 mL / min: Gradient: 0-1 min 5% B; 1-15 min 5-95% B; 15-20 min 95% B; 20-22 min 95-5% B; 22-25 min 95% B.

Analytical Method 2:

[0730]The system consisted of a Finnigan AQA single quadrupole mass spectrometer linked to a Hewlett Packard 1050 LC system with UV diode array detector and autosampler and using a Luna 3 μm C18(2) 30×4.6 mm column or equivalent. The spectrometer had an electrospray source operating in positive ion mo...

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PUM

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Abstract

The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain amido-isothiazole compounds that, inter alia, inhibit 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit 11β-hydroxysteroid dehydrogenase type 1; to treat disorders that are ameliorated by the inhibition of 11β-hydroxysteroid dehydrogenase type 1; to treat the metabolic syndrome, which includes disorders such as type 2 diabetes and obesity, and associated disorders including insulin resistance, hypertension, lipid disorders and cardiovascular disorders such as ischaemic (coronary) heart disease; to treat CNS disorders such as mild cognitive impairment and early dementia, including Alzheimer's disease; etc.

Description

RELATED APPLICATION[0001]This application is related to U.S. provisional patent application No. 61 / 186,963 filed 15 Jun. 2009, the contents of which are incorporated herein by reference in their entirety.TECHNICAL FIELD[0002]The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain amido-isothiazole compounds that, inter alia, inhibit 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit 11β-hydroxysteroid dehydrogenase type 1; to treat disorders that are ameliorated by the inhibition of 11β-hydroxysteroid dehydrogenase type 1; to treat the metabolic syndrome, which includes disorders such as type 2 diabetes and obesity, and associated disorders including insulin resistance, hypertension, lipid disorders and cardiovascular diso...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K31/4709C07D417/14A61K31/427C12N9/99A61P43/00A61P3/10A61P3/08A61P3/04A61P3/06A61P9/10A61P9/00A61P3/00A61P1/16A61P25/00A61P25/18A61P25/28A61P25/16A61P1/18A61P27/06A61P25/22A61P25/24A61P29/00A61P19/10A61P9/12A61P27/02A61P11/06A61P11/00A61P17/00A61P1/00A61P19/02C07D413/06
CPCC07D417/14C07D417/06A61P1/00A61P1/16A61P1/18A61P3/00A61P3/04A61P3/06A61P3/08A61P3/10A61P9/00A61P9/10A61P9/12A61P11/00A61P11/06A61P17/00A61P19/02A61P19/10A61P25/00A61P25/16A61P25/18A61P25/22A61P25/24A61P25/28A61P27/02A61P27/06A61P29/00A61P43/00
Inventor WEBSTER, SCOTT PETERSECKL, JONATHAN ROBERTWALKER, BRIAN ROBERTWARD, PETERPALLIN, THOMAS DAVIDDYKE, HAZEL JOANPERRIOR, TREVOR ROBERT
Owner THE UNIV COURT OF THE UNIV OF EDINBURGH
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